SPRAY DRYING APPROACH IN PREPARATION AND CHARACTERIZATION OF SOLID DISPERSION OF EPROSARTAN MESYLATE

Spray drying methods were used to make solid dispersions of the medication Eprosartan Mesylate, which is poorly water-soluble. X-ray Powder diffraction, Fourier transform infrared spectroscopy, and differential scanning calorimetry were used to characterize the products' physicochemical features as well as drug-polymer interactions. Eprosartan Mesylate was shown to be dispersed amorphously in both solid dispersion systems, with a drug to polymer weight ratio of 1:4.The drug and polymer created hydrogen bonds, according to the spectrum data. Both techniques utilized in this investigation enhanced Eprosartan Mesylate solubility. Solid dispersions, on the other hand, performed significantly better, dissolving completely in 5 minutes and at a rate that was about 20 times faster than API within the first 15 minutes. Spray drying is a good way to boost the bioavailability of drugs that are poor water solubility.

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Preparation and Characterization of Artemether Solid Dispersion by Spray Drying Technique

Journal of Drug Delivery and Therapeutics ◽

10.22270/jddt.v11i2.4557 ◽

2021 ◽

Vol 11 (2) ◽

pp. 1-5

Author(s):

Dhiraj Dabhade ◽

Kamlesh Wadher ◽

Shrikant Bute ◽

Nikita Naidu ◽

Milind Umekar ◽

...

Keyword(s):

Dissolution Rate ◽

Spray Drying ◽

Solid Dispersion ◽

Solid Dispersions ◽

Amorphous Solid ◽

Study Data ◽

Water Soluble ◽

Amorphous Solid Dispersion ◽

Scanning Calorimetry ◽

Poorly Water Soluble

Introduction: Artemether, a BCS class IV drug (poorly water soluble and poorly permeable, less bioavailability) but is found to be effective against falciparum malaria. Preparation of water soluble formulation could be the technique to improve bioavailability of such drug. The most ideally used technique to enhance the solubility and dissolution of poorly water soluble drugs is Solid dispersion method. Method: The objective of the study was to enhance the solubility and dissolution rate of Artemether by preparing solid dispersions using Soluplus, at different ration of 1:1, 1:2, 1:3 and 1:4 using spray drying technology. Prepared Solid dispersions were characterized by Fourier transform infrared spectroscopy and differential scanning calorimetry. Results: The spray-dried solid dispersions found to be having less crystallinity and showed higher dissolution rates. Solubility study data showed the optimum drug/Soluplus ratio to be 1:3. The dissolution studies of Solid dispersions in 1.2 pH and 6.8 pH buffer showed higher drug release as compared to pure drug. Conclusion: Thus we conclude that an amorphous solid dispersion of Artemether could be a better option for enhancing the dissolution rate of drug Keywords: solid dispersion, artemether, soluplus, solubility enhancement

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Solubility and Dissolution Enhancement of Atorvastatin Calcium using Solid Dispersion Adsorbate Technique

Iraqi Journal of Pharmaceutical Sciences ( P-ISSN 1683 - 3597 E-ISSN 2521 - 3512) ◽

10.31351/vol28iss2pp105-114 ◽

2019 ◽

Vol 28 (2) ◽

pp. 105-114

Author(s):

Samer K. Ali ◽

Eman B. H. Al-Khedairy

Keyword(s):

Polyethylene Glycol ◽

Solid Dispersion ◽

Water Solubility ◽

Drug Carrier ◽

Solid Dispersions ◽

Poloxamer 407 ◽

Dissolution Enhancement ◽

Drug Solubility ◽

Scanning Calorimetry ◽

Poorly Soluble

Atorvastatin (ATR) is poorly soluble anti-hyperlipidemic drug; it belongs to the class II group according to the biopharmaceutical classification system (BCS) with low bioavailability due to its low solubility. Solid dispersions adsorbate is an effective technique for enhancing the solubility and dissolution of poorly soluble drugs. The present study aims to enhance the solubility and dissolution rate of ATR using solid dispersion adsorption technique in comparison with ordinary solid dispersion. polyethylene glycol 4000 (PEG 4000), polyethylene glycol 6000 (PEG 6000), Poloxamer188 and Poloxamer 407were used as hydrophilic carriers and Aerosil 200, Aerosil 300 and magnesium aluminium silicate (MAS) as adsorbents. All solid dispersion adsorbate (SDA) formulas were prepared in ratios of 1:1:1 (drug: carrier: adsorbent) and evaluated for their water solubility, percentage yield, drug content, , dissolution, crystal structure using X-ray powder diffraction (XRD) and Differential Scanning Calorimetry (DSC) studies and Fourier Transform Infrared Spectroscopy (FTIR) for determination the drug-carrier- adsorbate interaction. The prepared (SDA) showed significant improvement of drug solubility in all prepared formula. Best result was obtained with formula SDA12(ATR :Poloxamer407 : MAS 1:1:1) that showed 8.07 and 5.38 fold increase in solubility compared to solubility of pure ATR and solid dispersion(SD4) (Atorvastatin: Poloxamer 407 1:1) respectively due to increased wettability and reduced crystallinity of the drug which leads to improve drug solubility and dissolution .

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Design and Characterization of Phosphatidylcholine-Based Solid Dispersions of Aprepitant for Enhanced Solubility and Dissolution

Pharmaceutics ◽

10.3390/pharmaceutics12050407 ◽

2020 ◽

Vol 12 (5) ◽

pp. 407

Author(s):

Sooho Yeo ◽

Jieun An ◽

Changhee Park ◽

Dohyun Kim ◽

Jaehwi Lee

Keyword(s):

Solid Dispersion ◽

Solid Dispersions ◽

Amorphous State ◽

Aqueous Solubility ◽

Water Soluble ◽

Scanning Calorimetry ◽

Promising Alternative ◽

Dispersion System ◽

Enhanced Solubility ◽

Water Soluble Drugs

This study aimed to improve the solubility and dissolution of aprepitant, a drug with poor aqueous solubility, using a phosphatidylcholine (PC)-based solid dispersion system. When fabricating the PC-based solid dispersion, we employed mesoporous microparticles, as an adsorbent, and disintegrants to improve the sticky nature of PC and dissolution of aprepitant, respectively. The solid dispersions were prepared by a solvent evaporation technique and characterized by Fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry, and X-ray powder diffraction. The FTIR results showed that aprepitant interacted with the PC carrier by both hydrogen bonds and van der Waals forces that can also be observed in the interaction between aprepitant and polymer carriers. The solid dispersions fabricated with only PC were not sufficient to convert the crystallinity of aprepitant to an amorphous state, whereas the formulations that included adsorbent and disintegrant successfully changed that of aprepitant to an amorphous state. Both the solubility and dissolution of aprepitant were considerably enhanced in the PC-based solid dispersions containing adsorbent and disintegrant compared with those of pure aprepitant and polymer-based solid dispersions. Therefore, these results suggest that our PC-based solid dispersion system is a promising alternative to conventional formulations for poorly water-soluble drugs, such as aprepitant.

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Preparation and evaluation of azithromycin binary solid dispersions using various polyethylene glycols for the improvement of the drug solubility and dissolution rate

Brazilian Journal of Pharmaceutical Sciences ◽

10.1590/s1984-82502016000100002 ◽

2016 ◽

Vol 52 (1) ◽

pp. 1-13 ◽

Cited By ~ 6

Author(s):

Ehsan Adeli

Keyword(s):

Dissolution Rate ◽

Solid Dispersion ◽

Solid Dispersions ◽

Water Soluble ◽

Polyethylene Glycols ◽

X Ray Diffraction ◽

Drug Release Profile ◽

Scanning Calorimetry ◽

Peg 4000 ◽

Poorly Soluble

ABSTRACT Azithromycin is a water-insoluble drug, with a very low bioavailability. In order to increase the solubility and dissolution rate, and consequently increase the bioavailability of poorly-soluble drugs (such as azithromycin), various techniques can be applied. One of such techniques is "solid dispersion". This technique is frequently used to improve the dissolution rate of poorly water-soluble compounds. Owing to its low solubility and dissolution rate, azithromycin does not have a suitable bioavailability. Therefore, the main purpose of this investigation was to increase the solubility and dissolution rate of azithromycin by preparing its solid dispersion, using different Polyethylene glycols (PEG). Preparations of solid dispersions and physical mixtures of azithromycin were made using PEG 4000, 6000, 8000, 12000 and 20000 in various ratios, based on the solvent evaporation method. From the studied drug release profile, it was discovered that the dissolution rate of the physical mixture, as the well as the solid dispersions, were higher than those of the drug alone. There was no chemical incompatibility between the drug and polymer from the observed Infrared (IR) spectra. Drug-polymer interactions were also investigated using Differential Scanning Calorimetry (DSC), Powder X-Ray Diffraction (PXRD) and Scanning Election Microscopy (SEM). In conclusion, the dissolution rate and solubility of azithromycin were found to improve significantly, using hydrophilic carriers, especially PEG 6000.

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Solid dispersion of meloxicam: Factorially designed dosage form for geriatric population

Acta Pharmaceutica ◽

10.2478/v10007-007-0048-y ◽

2008 ◽

Vol 58 (1) ◽

pp. 99-110 ◽

Cited By ~ 17

Author(s):

Deepa Pathak ◽

Sunita Dahiya ◽

Kamla Pathak

Keyword(s):

Drug Release ◽

Solid Dispersion ◽

Dosage Form ◽

Solid Dispersions ◽

Methyl Cellulose ◽

Water Soluble ◽

Hydroxyethyl Cellulose ◽

Scanning Calorimetry ◽

Geriatric Population ◽

Peg 4000

Solid dispersion of meloxicam: Factorially designed dosage form for geriatric populationThe objective of the present work was to improve the dissolution properties of the poorly water-soluble drug meloxicam by preparing solid dispersions with hydroxyethyl cellulose (HEC), mannitol and polyethylene glycol (PEG) 4000 and to develop a dosage form for geriatric population. Differential scanning calorimetry, X-ray diffractometry, Fourier transform infrared spectroscopy and scanning electron microscopy were used to investigate the solid-state physical structure of the prepared solid dispersions. Higher invitrodissolution of solid dispersions was recorded compared to their corresponding physical mixtures and the pure drug. PEG 4000 in 1: 9 drug to carrier ratio exhibited the highest drug release (100.2%), followed by mannitol (98.2%) and HEC (89.5%) in the same ratio. Meloxicam-PEG 4000 solid dispersion was formulated into suspension and optimization was carried out by 23factorial design. Formulations containing higher levels of methyl cellulose and higher levels of either sodium citrate or Tween 80 exhibited the highest drug release.

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DEVELOPMENT AND IN VITRO DISSOLUTION STUDY OF BINARY AND TERNARY SOLID DISPERSIONS OF ACECLOFENAC

Universal Journal of Pharmaceutical Research ◽

10.22270/ujpr.v4i1.240 ◽

2019 ◽

Author(s):

Md. Shahidul Islam ◽

Rasheda Akter Lucky

Keyword(s):

Polyethylene Glycol ◽

Dissolution Rate ◽

Solid Dispersion ◽

Drug Carrier ◽

Solid Dispersions ◽

Weight Ratio ◽

Water Soluble ◽

In Vitro Dissolution ◽

Peg 6000

The poor aqueous solubility of the drug exhibits in variable dissolution rate and hence poor bioavailability. Aceclofenac is poorly water soluble drug. The aim of the present study was to improve the water solubility and the dissolution rate of Aceclofenac by solid dispersion technique using different water soluble polymers. The term solid dispersions refer to the dispersions of one or more active ingredients in an inert carrier or matrix at solid state. In this study, binary solid dispersion of Aceclofenac were prepared by fusion method using Polyethylene glycol 6000 (PEG 6000), Polyethylene glycol 4000 (PEG 4000), Poloxamer as carrier. Different drug-carrier weight ratio was used for this study. The effect of the carrier on the solubility and in-vitro dissolution were studied. It was found the drug was released 26.86% after 5 minutes and only 40.19% within 60 mins from active Aceclofenac on the other hand the release pattern of Aceclofenac from the binary SD formulation containing PEG 6000 in 1:5 ratio (Formulation coding: A5) showed the best result in comparison of other binary and ternary SD formulations which was 62.29% after 5 min and 83.03% within 60 mins. The hydrophilic polymers used for the preparation of solid dispersion are showed significant increase in the solubility of Aceclofenac.

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DEVELOPMENT AND EVALUATION OF MONOLITHIC OSMOTIC TABLET OF KETOPROFEN: USING SOLID DISPERSION TECHNIQUE

International Journal of Pharmacy and Pharmaceutical Sciences ◽

10.22159/ijpps.2016v8i12.11437 ◽

2016 ◽

Vol 8 (12) ◽

pp. 41

Author(s):

S. Kaushik ◽

Kamla Pathak

Keyword(s):

Solid Dispersion ◽

Solid Dispersions ◽

Amorphous State ◽

Immediate Release ◽

Water Soluble ◽

Scanning Calorimetry ◽

Peg 6000 ◽

Environmental Media ◽

Dispersion Technique

Objective: The aim of the present study was to develop and evaluate the monolithic osmotic tablet (MOT) composed of the solid dispersion of ketoprofen (KETO), a poorly water-soluble drug. Solid dispersion technique is generally used for immediate release, as this maximizes the amount of drug absorbed. Sustained release may be obtained by combining solid dispersion technique with MOT so as to increase the therapy efficacy and patient compliance.Methods: Solid dispersion of KETO was prepared by using solvent melt method with polyethylene glycol (PEG) 6000, a hydrophilic carrier. The ratio of KETO to PEG 6000 were 1:1, 1:3 and 1:5 (%w/w). These solid dispersions were characterized by differential scanning calorimetry (DSC), Thermogravimetric analysis (TGA) and powder X-ray diffraction (PXRD) to ascertain whether there were any physicochemical interactions between drug and carrier.The tablet core was prepared by using Polyox N80 (a suspending agent), sodium chloride (an osmotic agent), a solid dispersion consisting of PEG 6000 and KETO followed by a coating of cellulose acetate to make the monolithic osmotic tablet.Results: The results of DSC and PXRD indicated that the drug was in the amorphous state in solid dispersion when PEG 6000 was used as a carrier. The dissolution rate of the solid dispersion was much faster than those for the corresponding physical mixture and pure drug. The optimized MOT formulations were able to deliver KETO at the constant zero order release, above 95% in vitro, independent to environmental media and stirring rate. The release rate of KETO in the MOT is controlled by osmotic pressure, suspending agent and drug solubility in solid dispersion.Conclusion: The monolithic osmotic tablet containing solid dispersion has great potential in the controlled delivery of ketoprofen, a water-insoluble drug.Keywords: Ketoprofen, Monolithic osmotic tablet, Solid dispersion, Water insoluble

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Increasing Solubility of Poorly Water Soluble Drug Resveratrol by Surfactants and Cyclodextrins

Advanced Materials Research ◽

10.4028/www.scientific.net/amr.418-420.2231 ◽

2011 ◽

Vol 418-420 ◽

pp. 2231-2234 ◽

Cited By ~ 7

Author(s):

Mont Kumpugdee-Vollrath ◽

Yvonne Ibold

Keyword(s):

Solid Dispersion ◽

Water Solubility ◽

Solid Dispersions ◽

Water Soluble ◽

Dispersion Phase ◽

Water Soluble Drug ◽

Vis Spectroscopy ◽

Anti Cancer ◽

Cancer Agent ◽

Span 60

Resveratrol (Res) is a polyphenolic secondary natural substance and can be used as anti-inflammatory, anti-aging, anti-heart disease and anti-cancer agent. However, Res has low water solubility which causes a low bioavailability in human body. In order to increase solubility we have prepared different inclusion complexes with native ((α, β, γ) and modified (2-hydroxypropyl-beta, dimethyl-beta) cyclodextrins (Cd) as well as solid dispersions using several surfactants (Imwitor 742, Imwitor 928, PEG 6000, Span 40, Span 60, Solutol HS15) with Res. The solubility of all mixtures was determined by UV-VIS spectroscopy at the wavelength of 305 nm. Regarding the Cd, the complex of Res with 2-hydroxypropyl-beta-Cd at a ratio of 1:3 showed the highest water solubility (248210 g/l). Concerning the surfactants, the solid dispersion from Res and Solutol HS15 showed the highest water solubility (16140 g/l). The complexation and the solid dispersion phase were confirmed by DSC. The results will be a basis for better formulation of resveratrol with higher bioavailability.

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Improvement in Dissolution of Bosentan Monohydrate by Solid Dispersions Using Spray Drying Technique

Open Pharmaceutical Sciences Journal ◽

10.2174/1874844901704010023 ◽

2017 ◽

Vol 4 (1) ◽

pp. 23-31 ◽

Cited By ~ 3

Author(s):

Pankaj V. Dangre ◽

Vikesh B. Sormare ◽

Mangesh D. Godbole

Keyword(s):

Spray Drying ◽

Solid Dispersion ◽

Large Scale ◽

Solid Dispersions ◽

Significant Rise ◽

Water Soluble ◽

Drug Dissolution ◽

Absolute Bioavailability ◽

Water Soluble Drug ◽

Peg 4000

Background: Bosentan monohydrate (BM), a dual endothelin receptor antagonist, is indicated for the treatment of patients with pulmonary arterial hypertension (PAH). It is poorly soluble in water, and having absolute bioavailability of 50%. Objective: The aim of the present work is to develop and evaluate the solid dispersions (SD) of a poorly water soluble drug bosentan monohydrate (BM). Method: Solid dispersions (SDs) systems of BM were prepared with Hydroxy propyle β-cyclodextrin (HPβ-CD) and Polyethylene glycol (PEG-4000) polymers using a spray drying technique. Result: The significant rise in a saturation solubility 174.23±1.36 mg/mL; and drug dissolution 95.11±1.22%; was observed with optimized formulation (SD 6). The solid state characterization of optimized formulation (SD 6) by SEM, DSC, and XRPD revealed the absence of crystalline nature of BM in solid dispersion. High dissolution rate of solid dispersion (SD 6) compared with pure drug indicated the increase in dissolution characteristics. Conclusion: In conclusion, our studies illustrated that spray drying technique could be useful large scale producing method to prepare the solid dispersion of bosentan with HP β-CD, which can improve the solubility as well as stability of the formulation.

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SOLUBILITY ENHANCEMENT OF POOR WATER SOLUBLE DRUGS BY SOLID DISPERSION: A REVIEW

Journal of Drug Delivery and Therapeutics ◽

10.22270/jddt.v8i5.1887 ◽

2018 ◽

Vol 8 (5) ◽

pp. 44-49 ◽

Cited By ~ 1

Author(s):

SD Mankar ◽

Punit R. Rach

Keyword(s):

Solid Dispersion ◽

High Throughput Screening ◽

Water Solubility ◽

Solid Dispersions ◽

Scale Up ◽

Solubility Enhancement ◽

Water Soluble ◽

Formulation Development ◽

Solubility Behavior ◽

Poorly Water Soluble

The solubility behavior of drugs remains one of the most exigent aspects in formulation development. With the advent of combinatorial chemistry and high throughput screening, the number of poorly water soluble compounds has dramatically increased. Among all the newly discovered chemical entities, about 40-45% drugs fail to reach market due to their poor water solubility. Because of solubility problem, bioavailability of drugs gets affected and hence solubility enhancement becomes necessary. Solid dispersions have attracted considerable interest as an efficient means of improving the dissolution rate and hence the bioavailability of drugs. Therefore, the application of this technique proves to be an important stratagem for pharmaceutical companies. However, the in - depth knowledge of the solid dispersion is desired for the scale up of formulation, from laboratory scale to industrial scale. There are various methods available to improve the solubility of the new drug in which solid dispersion emerged promising. A Solid dispersion generally composed of two components- the drug and the polymer matrix. Hence, this approach is expected to form a basis for the commercialization of many poorly water-soluble and water-insoluble drugs in their solid-dispersion formulations in the near future. This article reviews the various preparation techniques, carriers used, advantages and limitations of solid dispersions and compiles some of the recent advances. Keywords: Bioavailability, Solid Dispersion, Hydrophilic carriers, Polyethylene glycol.

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